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    COMPOUNDS FOR BINDING TO ER ALPHA/BETA AND GPR30, METHODS OF TREATING DISEASE STATES AND CONDITIONS MEDIATED THROUGH THESE RECEPTORS AND IDENTIFICATION THEREOF
    33.
    发明申请
    COMPOUNDS FOR BINDING TO ER ALPHA/BETA AND GPR30, METHODS OF TREATING DISEASE STATES AND CONDITIONS MEDIATED THROUGH THESE RECEPTORS AND IDENTIFICATION THEREOF 有权
    用于与ALPHA / BETA和GPR30结合的化合物，通过这些受体介导的治疗疾病状态的方法和鉴定方法

    公开(公告)号：US20110092533A1

    公开(公告)日：2011-04-21

    申请号：US12967871

    申请日：2010-12-14

    申请人： Eric R. PROSSNITZ ,  Sergey E. Tkatchenko ,  Chetana M. Revankar ,  Larry A. Sklar ,  Jeffrey B. Arterburn ,  Daniel F. Cimino ,  Tudor I. Oprea ,  Cristian-George Bologa ,  Bruce S. Edwards ,  Alexander Kiselyov ,  Susan M. Young

    发明人： Eric R. PROSSNITZ ,  Sergey E. Tkatchenko ,  Chetana M. Revankar ,  Larry A. Sklar ,  Jeffrey B. Arterburn ,  Daniel F. Cimino ,  Tudor I. Oprea ,  Cristian-George Bologa ,  Bruce S. Edwards ,  Alexander Kiselyov ,  Susan M. Young

    IPC分类号： A61K31/435 ,  C07D405/10 ,  C07D221/16 ,  C07D405/14 ,  A61P43/00

    CPC分类号： C07D221/16 ,  C07D405/04 ,  C07D405/14

    摘要： The current invention is in the field of molecular biology/pharmacology and provides compounds which modulate the effects of GPR30 as well as the classical estrogen receptors alpha and beta (ERα and ERβ). These compounds may function as agonists and/or antagonists of one or more of the disclosed estrogen receptors. Diseases which are mediated through one or more of these receptors include cancer (particularly breast, reproductive and other hormone-dependent cancers, leukemia, colon cancer, prostate cancer), reproductive (genito-urological) including endometreitis, prostatitis, polycystic ovarian syndrome, bladder control, hormone-related disorders, hearing disorders, cardiovascular conditions including hot flashes and profuse sweating, hypertension, stroke, obesity, osteoporosis, hematologic diseases, vascular diseases or conditions such as venous thrombosis, atherosclerosis, among numerous others and disorders of the central and peripheral nervous system, including depression, insomnia, anxiety, multiple sclerosis, neuropathy, neurodegenerative disoders such as Parkinson's disease and Alzheimer's disease, as well as inflammatory bowel disease, Crohn's disease, coeliac (celiac) disease and related disorders of the intestine. A contraceptive indication to prevent or reduce the likelihood of pregnancy after intercourse is a further aspect of the present invention.

    摘要翻译： 本发明在分子生物学/药理学领域，并提供调节GPR30以及经典雌激素受体α和β（ERα和ER和bgr）的作用的化合物。 这些化合物可以用作一种或多种所公开的雌激素受体的激动剂和/或拮抗剂。 通过这些受体中的一种或多种介导的疾病包括癌症（特别是乳腺，生殖和其他激素依赖性癌症，白血病，结肠癌，前列腺癌），生殖（泌尿 - 泌尿）包括子宫内膜炎，前列腺炎，多囊卵巢综合征，膀胱 控制，激素相关疾病，听觉障碍，心血管疾病，包括潮热和大量出汗，高血压，中风，肥胖，骨质疏松症，血液病，血管疾病或诸如静脉血栓形成，动脉粥样硬化等疾病，以及许多其他疾病和中枢和 周围神经系统，包括抑郁症，失眠，焦虑，多发性硬化，神经病变，神经变性解码器如帕金森病和阿尔茨海默病，以及炎性肠病，克罗恩病，腹腔（腹腔）疾病和肠道相关疾病。 用于预防或减少性交后怀孕的可能性的避孕指示是本发明的另一方面。

    Inhibition of cell surface protein disulfide isomerase
    37.
    发明授权
    Inhibition of cell surface protein disulfide isomerase 失效
    抑制细胞表面蛋白二硫键异构酶

    公开(公告)号：US06949665B2

    公开(公告)日：2005-09-27

    申请号：US10002698

    申请日：2001-12-05

    申请人： Snezna Rogelj ,  Larry A. Sklar ,  Robert B. Palmer

    发明人： Snezna Rogelj ,  Larry A. Sklar ,  Robert B. Palmer

    IPC分类号： A61K31/285 ,  A61K31/42 ,  A61K31/555 ,  C07F9/70

    CPC分类号： A61K31/555 ,  A61K31/285 ,  A61K31/42

    摘要： The invention provides anti-thiol reagents which inhibit enzyme activity of cell-associated protein disulfide isomerase (PDI) by oxidizing or blocking PDI active site vicinal thiol groups which normally participate in disulfide bond rearrangement of PDI substrates. Inhibition of this PDI function is particularly useful in blocking PDI-mediated entry of HIV or other virions into a host cell, as well as inhibiting lymphocyte traffic through the lymph nodes. The invention further provides an assay for the identification of such PDI inhibitors based on the discovery that inhibitors of the invention also induce shedding of the leucocyte L-selectin adhesion molecule.

    摘要翻译： 本发明提供通过氧化或阻断通常参与PDI底物的二硫键重排的PDI活性位点连位硫醇基团来抑制细胞相关蛋白二硫键异构酶（PDI）的酶活性的抗硫醇试剂。 该PDI功能的抑制特别可用于阻断PDI介导的HIV或其它病毒体进入宿主细胞，以及抑制通过淋巴结的淋巴细胞流量。 基于本发明的抑制剂还诱导白细胞L-选择素粘附分子的脱落的发现，本发明还提供了用于鉴定这种PDI抑制剂的测定法。

    Method for induction of L-selectin shedding
    39.
    发明授权
    Method for induction of L-selectin shedding 失效
    诱导L-选择蛋白脱落的方法

    公开(公告)号：US06498189B1

    公开(公告)日：2002-12-24

    申请号：US09442940

    申请日：1999-11-18

    申请人： Snezna Rogelj ,  Teresa A. Bennett ,  Larry A. Sklar

    发明人： Snezna Rogelj ,  Teresa A. Bennett ,  Larry A. Sklar

    IPC分类号： A61K31285

    CPC分类号： A61K31/285

    摘要： The invention provides anti-thiol reagents which inhibit enzyme activity of cell-associated protein disulfide isomerase (PDI) by oxidizing or blocking PDI active site vicinal thiol groups which normally participate in disulfide bond rearrangement of PDI substrates. Inhibition of this PDI function is particularly useful in blocking PDI-mediated entry of HIV or other virions into a host cell, as well as inhibiting lymphocyte traffic through the lymph nodes. The invention further provides an assay for the identification of such PDI inhibitors based on the discovery that inhibitors of the invention also induce shedding of the leucocyte L-selectin adhesion molecule. The invention additionally provides for suppression of inflammation and of lymph node entry by calmodulin antagonists that, like PDI inhibition, cause leukocyte L-selectin shedding.

    摘要翻译： 本发明提供通过氧化或阻断通常参与PDI底物的二硫键重排的PDI活性位点连位硫醇基团来抑制细胞相关蛋白二硫键异构酶（PDI）的酶活性的抗硫醇试剂。 该PDI功能的抑制特别可用于阻断PDI介导的HIV或其它病毒体进入宿主细胞，以及抑制通过淋巴结的淋巴细胞流量。 基于本发明的抑制剂还诱导白细胞L-选择素粘附分子的脱落的发现，本发明还提供了用于鉴定这种PDI抑制剂的测定法。 本发明另外提供抑制钙调素拮抗剂的炎症和淋巴结进入，其像PDI抑制一样导致白细胞L-选择蛋白脱落。